Development of in situ gelling and bio adhesive 5-Fluorouracil enema.

In this study, a novel 5-Fluorouracil (5-FU) enema with good bio adhesion and temperature sensitivity was developed using in situ gelling technology. The preparation was formulated as a free-flowing liquid before use, while a layer of gel film was quickly formed when administered in the rectum, with...

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Autores principales:	Lu-Lu Wang, Wen-Sheng Zheng, Shao-Hua Chen, Xia-Qin Fang
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2013
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/f679d261cae942fd8ac0d803fd845262
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spelling	oai:doaj.org-article:f679d261cae942fd8ac0d803fd8452622021-11-18T08:59:19ZDevelopment of in situ gelling and bio adhesive 5-Fluorouracil enema.1932-620310.1371/journal.pone.0071037https://doaj.org/article/f679d261cae942fd8ac0d803fd8452622013-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/23976976/pdf/?tool=EBIhttps://doaj.org/toc/1932-6203In this study, a novel 5-Fluorouracil (5-FU) enema with good bio adhesion and temperature sensitivity was developed using in situ gelling technology. The preparation was formulated as a free-flowing liquid before use, while a layer of gel film was quickly formed when administered in the rectum, with a large contact surface area. It also demonstrated good biocompatibility, appropriate gel strength and bio adhesive force with excellent adhesion to rectal mucosa and prolonged action time, allowing more effective drug absorption and diffusion to surrounding tissues. Poloxamer 407 and poloxamer 188 were applied to adjust the gelling temperature. With the addition of carbopol and polycarbophil (bio adhesive substances), the solubility of 5-FU and gel strength increased, the temperature of gelation and the surface area of drug contact on mucous epithelium decreased. Decreased adhesive force between the preparation and the mucous membrane of the rectum was demonstrated with improving carbopol and polycarbophil's concentration. In vitro release demonstrated that 5-FU in situ gelling enema with different bases had a rapid and almost complete drug release. We used an optimized formulation of P407/P188/polycarbophil/5-FU (17/2.5/0.2/1.0) for animal experiments. The result showed that the drug evenly covered the surface of the rectum and there was no leakage in 6 hours. The in situ gelling enema showed significantly higher rectal tissue levels of 5-FU compared with suppository and intravenous administration, indicating that 5-FU could be well absorbed due to the enlarged releasing area, longer retention time and larger amount of dissolved active ingredients. Systemically, 5-FU levels in the enema group were similar to those in the suppository group and significantly lower than the intravenous group. The enema was not associated with morphological damage to rectal tissue. These results suggest that the bio adhesive and in situ gelling enema could be a more effective rectal delivery system of 5-FU.Lu-Lu WangWen-Sheng ZhengShao-Hua ChenXia-Qin FangPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 8, Iss 8, p e71037 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Lu-Lu Wang Wen-Sheng Zheng Shao-Hua Chen Xia-Qin Fang Development of in situ gelling and bio adhesive 5-Fluorouracil enema.
description	In this study, a novel 5-Fluorouracil (5-FU) enema with good bio adhesion and temperature sensitivity was developed using in situ gelling technology. The preparation was formulated as a free-flowing liquid before use, while a layer of gel film was quickly formed when administered in the rectum, with a large contact surface area. It also demonstrated good biocompatibility, appropriate gel strength and bio adhesive force with excellent adhesion to rectal mucosa and prolonged action time, allowing more effective drug absorption and diffusion to surrounding tissues. Poloxamer 407 and poloxamer 188 were applied to adjust the gelling temperature. With the addition of carbopol and polycarbophil (bio adhesive substances), the solubility of 5-FU and gel strength increased, the temperature of gelation and the surface area of drug contact on mucous epithelium decreased. Decreased adhesive force between the preparation and the mucous membrane of the rectum was demonstrated with improving carbopol and polycarbophil's concentration. In vitro release demonstrated that 5-FU in situ gelling enema with different bases had a rapid and almost complete drug release. We used an optimized formulation of P407/P188/polycarbophil/5-FU (17/2.5/0.2/1.0) for animal experiments. The result showed that the drug evenly covered the surface of the rectum and there was no leakage in 6 hours. The in situ gelling enema showed significantly higher rectal tissue levels of 5-FU compared with suppository and intravenous administration, indicating that 5-FU could be well absorbed due to the enlarged releasing area, longer retention time and larger amount of dissolved active ingredients. Systemically, 5-FU levels in the enema group were similar to those in the suppository group and significantly lower than the intravenous group. The enema was not associated with morphological damage to rectal tissue. These results suggest that the bio adhesive and in situ gelling enema could be a more effective rectal delivery system of 5-FU.
format	article
author	Lu-Lu Wang Wen-Sheng Zheng Shao-Hua Chen Xia-Qin Fang
author_facet	Lu-Lu Wang Wen-Sheng Zheng Shao-Hua Chen Xia-Qin Fang
author_sort	Lu-Lu Wang
title	Development of in situ gelling and bio adhesive 5-Fluorouracil enema.
title_short	Development of in situ gelling and bio adhesive 5-Fluorouracil enema.
title_full	Development of in situ gelling and bio adhesive 5-Fluorouracil enema.
title_fullStr	Development of in situ gelling and bio adhesive 5-Fluorouracil enema.
title_full_unstemmed	Development of in situ gelling and bio adhesive 5-Fluorouracil enema.
title_sort	development of in situ gelling and bio adhesive 5-fluorouracil enema.
publisher	Public Library of Science (PLoS)
publishDate	2013
url	https://doaj.org/article/f679d261cae942fd8ac0d803fd845262
work_keys_str_mv	AT luluwang developmentofinsitugellingandbioadhesive5fluorouracilenema AT wenshengzheng developmentofinsitugellingandbioadhesive5fluorouracilenema AT shaohuachen developmentofinsitugellingandbioadhesive5fluorouracilenema AT xiaqinfang developmentofinsitugellingandbioadhesive5fluorouracilenema
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Development of in situ gelling and bio adhesive 5-Fluorouracil enema.

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